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Literature summary for 2.7.1.151 extracted from

  • Mayr, G.W.; Windhorst, S.; Hillemeier, K.
    Antiproliferative plant and synthetic polyphenolics are specific inhibitors of vertebrate inositol-1,4,5-trisphosphate 3-kinases and inositol polyphosphate multikinase (2005), J. Biol. Chem., 280, 13229-13240.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type enzyme and deletion mutant in Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information construction of an N-terminal deletion mutant comprising residues 266-371, the mutant enzyme is inhibited by aurintricarboxylic acid, gossypol, 3',4',7,8-tetrahydroxyflavone, epigallocatechin-3-gallate, chlorogenic acid, and rose bengal, but not by quercetin, epicatechin-3-gallate, ellagic acid, hypericin, and myricetin in contrary to the wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
aurintricarboxylic acid mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, strong inhibition, IC50 is 44 nM Homo sapiens
chlorogenic acid mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0012 mM Homo sapiens
ellagic acid mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0014 mM Homo sapiens
gossypol mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0034 mM Homo sapiens
additional information inhibitory effects are not due to inactivating aggregation of the enzyme, no inhibition by quercetin, 3',4',7,8-tetrahydroxyflavone, myricetin, hypericin, epigallocatechin-3-gallate, and epicatechin-3-gallate, the enzyme contains a unique basic segment of 105 amino acids, which is inserted between the SSLL motif and the DFG motif, being probably involved in inhibition by acidic polyphenols Homo sapiens
Rose bengal mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 620 nM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00035
-
1D-myo-inositol 1,4,5-trisphosphate recombinant wild-type enzyme, pH 7.5, 30°C Homo sapiens
0.0004
-
1D-myo-inositol 1,4,5-trisphosphate recombinant deletion mutant enzyme, pH 7.5, 30°C Homo sapiens
0.017
-
ATP recombinant wild-type enzyme, pH 7.5, 30°C Homo sapiens
0.039
-
ATP recombinant deletion mutant enzyme, pH 7.5, 30°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus the enzyme contains a unique basic segment of 105 amino acids, which is inserted between the SSLL motif and the DFG motif, being responsible for nuclear localization and is probably also involved in inhibition by acidic polyphenols Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens
additional information free enzyme and inhibited enzyme are not affected by Ca2+ Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + 1D-myo-inositol 1,4,5-trisphosphate Homo sapiens
-
ADP + 1D-myo-inositol 1,4,5,6-tetrakisphosphate
-
?
additional information Homo sapiens the enzyme might be involved in regulation of cell growth ?
-
?

Organic Solvent Stability

Organic Solvent Comment Organism
additional information enzyme is not affected by 3% v/v DMSO Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant wild-type enzyme and deletion mutant from Escherichia coli by ion exchange and phosphocellulose resin chromatography Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.5
-
recombinant wild-type enzyme, substrate 1D-myo-inositol 1,4,5-trisphosphate Homo sapiens
5.5
-
recombinant deletion mutant enzyme, substrate 1D-myo-inositol 1,4,5-trisphosphate Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 1D-myo-inositol 1,4,5-trisphosphate
-
Homo sapiens ADP + 1D-myo-inositol 1,4,5,6-tetrakisphosphate
-
?
additional information the enzyme might be involved in regulation of cell growth Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
inositol polyphosphate multikinase
-
Homo sapiens
IPMK
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000044
-
mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, strong inhibition, IC50 is 44 nM Homo sapiens aurintricarboxylic acid
0.00062
-
mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 620 nM Homo sapiens Rose bengal
0.0012
-
mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0012 mM Homo sapiens chlorogenic acid
0.0014
-
mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0014 mM Homo sapiens ellagic acid
0.0034
-
mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate, slight inhibition, IC50 is 0.0034 mM Homo sapiens gossypol